Biological Information

Background Information:

Glucagon is an important hormone involved in carbohydrate metabolism. Produced by the pancreas, it is released when the glucose level in the blood is low (hypoglycemia) and major effect of glucagon is to stimulate an increase in blood concentration of glucose. The glucagon receptor is a 62 kDa peptide that is activated by glucagon and is a member of the G-protein coupled family of receptors, coupled to Gs. Stimulation of the receptor results in activation of adenylate cyclase and increased levels of intracellular cAMP. Glucagon receptors are mainly expressed in liver and in kidney with lesser amounts found in heart, adipose tissue, spleen, thymus, adrenal glands, pancreas, cerebral cortex, and gastrointestinal tract.

cAMP Hunter™ Gs cell lines overexpress naturally Gs coupled, wild type GPCRs and are designed to detect increases in intracellular cAMP levels in response to agonist stimulation of the receptor. These cell lines are designed to be used in conjunction with the HitHunter® cAMP Assay Detection Kit.

Family:

GPCR

Sub Family:

Glucagon

Class:

Class B

Coupling:

Gs

Protein Name:

Glucagon

Uniprot Number:

P47871

Gene Name:

GCGR

Gene ID:

2642

Gene Aliases:

GGR

Accession Number:

NM_000160

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Testing Information

Control Inhibitor:

[Des-His1, Glu9]-Glucagon amide

Control Activator:

Glucagon

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

Adverse / Beneficial Action:

Antagonizing the glucagon receptor is expected to result in reduced hepatic glucose overproduction, leading to overall glycemic control. Glucagon receptor antagonists could be an effective approach for controlling blood glucose in diabetes.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA